c-Fms

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation.

JNJ-6204 is a dual inhibitor of CSNK1D (IC50 = 2.3 nM) and CSNK1E (IC50 = 137 nM).

Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Pimicotinib (ABSK021) is a potent CSF1R inhibitor with antitumor activity and can be used to study advanced solid tumors.

GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS.

Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

CSF1R-IN-1 is a CSF1R inhibitor with an IC50 of 0.5 nM.

Vimseltinib (DCC-3014) is a dual inhibitor targeting c-FMS (CSF-IR) and c-Kit with IC50 values of less than 0.01 μM and 0.1-1 μM, respectively.

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

Lenzilumab (KB 003) is a humanized granulocyte-macrophage colony-stimulating factor (GM-CSF) neutralizing antibody that directly binds to GM-CSF and prevents signaling through its receptor, and can be used to study COVID-19.

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

Emactuzumab(RG 7155) is a monoclonal antibody against colony-stimulating factor-1 receptor targeting tumor-associated macrophages (TAMs) Emactuzumab has antitumor activity and inhibits activation of colony-stimulating factor 1 receptor (CSF1R) Emactuzumab has a high affinity for CSF-1R with a Ki value of 0.2 nM. Emactuzumab blocks CSF-1R dimerization and can be used to study cancers such as diffuse tenosynovial giant cell tumor (dt-GCT).

c-Fms-IN-1 is an inhibitor of c-FMS kinase (IC50 = 0.8 nM).

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

c-Fms-IN-2 is an inhibitor of c-FMS kinase (IC50 = 24 nM).

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).

AEE788 (NVP-AEE 788) has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

Anumigilimab (CSL-324) is a fully human therapeutic anti-G-CSFR antibody with potential anti-tumor activity for the study of inflammation.

Mavrilimumab (CAM 3001) is a monoclonal antibody with antiviral activity that targets the α subunit of the granulocytic-macrophage colony-stimulating factor (GM-CSF) receptor, inhibiting downstream intracellular GM-CSF signaling. GM-CSF may contribute to an overactive inflammatory response linked to respiratory failure and death and could be used to study rheumatoid arthritis.